1384517-65-0Relevant articles and documents
[18F] DPA-714 (N, N-diethyl-2-(2-(4-(2-[18]F-fluoroethyoxy)phenyl)-5, 7-dimethylpyrazolo[1, 5-a]pyrimidin-3-yl)aceamide) derivative and preparation and application methods thereof
-
Paragraph 0076; 0078; 0082, (2019/05/22)
The invention discloses a [18F] DPA-174 derivative. The [18F] DPA-174 derivative is prepared by modifying the benzene ring structure of or prolonging the carbon chain structure of a [18]F DPA-174 imaging agent. The invention also discloses preparation and application methods of the [18F] DPA-174 derivative. The [18F] DPA-174 derivative is simple in preparation, easy to implement, high in labellingyield and good in repeatability and can help in real time observe and in vivo monitor the status of intracerebral neuroinflammation of an animal model as well as the changes of the major organs and tissues of the animal model; the prepared imaging agents can achieve imaging effects on neuroinflammation; the [18F] DPAF imaging agent can achieve a high signal-to-noise ratio on neuroinflammation lesions to provide possibility for further monitoring and assessing the diagnosis and treatment effects on neuroinflammation..
Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)
Banister, Samuel D.,Beinat, Corinne,Wilkinson, Shane M.,Shen, Bin,Bartoli, Cecilia,Selleri, Silvia,Da Pozzo, Eleonora,Martini, Claudia,Chin, Frederick T.,Kassiou, Michael
, p. 392 - 400 (2015/03/04)
Sixteen new phenyl alkyl ether derivatives (12, 14-28) of the 5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-ylacetamide (DPA) class were synthesized and evaluated in a competition binding assay against [3H]PK11195 using 18 kDa translocator protein (TSPO) derived from rat kidney mitochondrial fractions. All analogues showed superior binding affinities for TSPO compared to DPA-713 (5) and DPA-714 (6). Picomolar affinities were observed for this class of TSPO ligands in this assay for the first time, with phenethyl ether 28 showing the greatest affinity (Ki Combining double low line 0.13 nM). Additionally, all analogues increased pregnenolone biosynthesis (134-331% above baseline) in a rat C6 glioma cell steroidogenesis assay.